Abstract
Dipeptides containing D‐phenylglycine or D‐p‐hydroxyphenylglycine were attached onto the antihypertensive agent α‐methyldopa to form prodrugs 1a, 1b and 1c. The nonessential amino acids were introduced into the prodrug molecules as tools of chemical delivery to improve the intestinal absorption of the parent drug. Preliminary tests revealed that the prodrugs were stable in phosphate buffer solutions at pH 7.4 (t1/2 > 10 h). These compounds also demonstrated satisfactory stability toward enzymatic degradation in a mucosa preparation isolated from rat intestine, indicating that they might be feasibly formulated as an oral prodrug of α‐methyldopa.
| Original language | English |
|---|---|
| Pages (from-to) | 561-567 |
| Number of pages | 7 |
| Journal | Journal of the Chinese Chemical Society |
| Volume | 42 |
| Issue number | 3 |
| DOIs | |
| Publication status | Published - 1995 |
| Externally published | Yes |
Fingerprint
Keywords
- Dipeptides as tools for intestinal delivery
- α‐Methyldopa prodrugs
ASJC Scopus subject areas
- Chemistry(all)
Cite this
Synthesis of α‐Methyldopa Prodrugs Containing Dipeptide Moieties as Tools for Intestinal Delivery. / Wang, Hui‐Po ‐P; Cheng, Chih‐Yuan ‐Y; Ma, Jin‐Ran ‐R; Lee, Jia‐Shuai ‐S.
In: Journal of the Chinese Chemical Society, Vol. 42, No. 3, 1995, p. 561-567.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Synthesis of α‐Methyldopa Prodrugs Containing Dipeptide Moieties as Tools for Intestinal Delivery
AU - Wang, Hui‐Po ‐P
AU - Cheng, Chih‐Yuan ‐Y
AU - Ma, Jin‐Ran ‐R
AU - Lee, Jia‐Shuai ‐S
PY - 1995
Y1 - 1995
N2 - Dipeptides containing D‐phenylglycine or D‐p‐hydroxyphenylglycine were attached onto the antihypertensive agent α‐methyldopa to form prodrugs 1a, 1b and 1c. The nonessential amino acids were introduced into the prodrug molecules as tools of chemical delivery to improve the intestinal absorption of the parent drug. Preliminary tests revealed that the prodrugs were stable in phosphate buffer solutions at pH 7.4 (t1/2 > 10 h). These compounds also demonstrated satisfactory stability toward enzymatic degradation in a mucosa preparation isolated from rat intestine, indicating that they might be feasibly formulated as an oral prodrug of α‐methyldopa.
AB - Dipeptides containing D‐phenylglycine or D‐p‐hydroxyphenylglycine were attached onto the antihypertensive agent α‐methyldopa to form prodrugs 1a, 1b and 1c. The nonessential amino acids were introduced into the prodrug molecules as tools of chemical delivery to improve the intestinal absorption of the parent drug. Preliminary tests revealed that the prodrugs were stable in phosphate buffer solutions at pH 7.4 (t1/2 > 10 h). These compounds also demonstrated satisfactory stability toward enzymatic degradation in a mucosa preparation isolated from rat intestine, indicating that they might be feasibly formulated as an oral prodrug of α‐methyldopa.
KW - Dipeptides as tools for intestinal delivery
KW - α‐Methyldopa prodrugs
UR - http://www.scopus.com/inward/record.url?scp=84986516348&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84986516348&partnerID=8YFLogxK
U2 - 10.1002/jccs.199500074
DO - 10.1002/jccs.199500074
M3 - Article
AN - SCOPUS:84986516348
VL - 42
SP - 561
EP - 567
JO - Journal of the Chinese Chemical Society
JF - Journal of the Chinese Chemical Society
SN - 0009-4536
IS - 3
ER -